The construction, prediction and measurement of co-crystal ternary phase diagrams as a tool for solvent selection
Language English Country Netherlands Media print-electronic
Document type Journal Article, Research Support, Non-U.S. Gov't
PubMed
24995701
DOI
10.1016/j.ejps.2014.06.017
PII: S0928-0987(14)00277-2
Knihovny.cz E-resources
- Keywords
- Agomelatine, Co-crystal, DITA, Solubility, Ternary phase diagram,
- MeSH
- Calorimetry MeSH
- Crystallization MeSH
- Citric Acid chemistry MeSH
- Pharmaceutical Preparations chemistry MeSH
- Solvents chemistry MeSH
- Solubility MeSH
- Temperature MeSH
- Publication type
- Journal Article MeSH
- Research Support, Non-U.S. Gov't MeSH
- Names of Substances
- Citric Acid MeSH
- Pharmaceutical Preparations MeSH
- Solvents MeSH
Many active pharmaceutical ingredients (APIs) are poorly soluble and therefore poorly bioavailable. In recent years, the advances in crystal engineering have motivated the research in the design of pharmaceutical co-crystals. This study examines the combination of solvent selection and co-crystal ternary phase diagram prediction on the basis of solubility measurements into a single methodology that can be integrated into the pharmaceutical process development workflow. Ternary diagrams constructed from agomelatine citric acid co-crystal solubility data were compared with those obtained by modern calorimetric method called discontinuous isoperibolic thermal analysis (DITA). A suitable solvent for the co-crystallization process has been chosen on the basis of agomelatine citric acid co-crystal solubility, which is connected to the yield of the crystallization process. Furthermore, the quality of final crystals from crystallization experiments was evaluated.
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References provided by Crossref.org
Surface Defects and Crystal Growth of Apremilast Benzoic Acid Cocrystals